📜正丁基硼酸置于potassium Hydrogen Bifluoride体系中,用 四氢呋喃 作为反应溶剂,以90%的收率获得产物丁基三氟硼酸钾 参考文献:Noncovalent Inhibition Of The Serine Proteases,α-Chymotrypsin And Trypsin By Trifluoro(Organo)Borates 标题:Noncovalent Inhibition Of The Serine Proteases,α-Chymotrypsin And Trypsin By Trifluoro(Organo)Borates 摘要:合成了一系列有机三氟硼酸钾.测定了它们在 D2O,Tris 和磷酸盐缓冲液中的水解稳定性.结果发现,在 D2O 和 Tris 缓冲液中,这些化合物都相当稳定,而在磷酸盐缓冲液中则会发生快速水解.基于这些结果,研究人员开始研究有机三氟硼酸钾是否可以作为蛋白酶抑制剂.研究发现,与相应的硼酸盐相比,有机三氟硼酸钾的抑制作用至少增加了一个数量级.狄克逊图显示,这些化合物是δ-糜蛋白酶和胰蛋白酶的可逆竞争抑制剂.根据 19F NMR,我们推测它们之所以能使酶失活,是因为抑制剂的氟原子与丝氨酸蛋白酶之间形成了氢键. DOI:10.1039/b415957H
专利号:US-8513465-B2 优先权日:2008-02-04 标题:Potassium organotrifluoroborate derivative and a production method therefor 发明人:KANG HEONJOONG; HAM JUNGYEOB; AHN HONG RYUL; PARK YOUNG HEE 权利人:KANG HEONJOONG; HAM JUNGYEOB; AHN HONG RYUL; PARK YOUNG HEE; SNU R&DB FOUNDATION 摘要:Provided are a production method for a potassium organotrifluoroborate compound having a hydroxyl group, and a novel potassium organotrifluoroborate compound having a hydroxyl group. The production method is advantageous in that a potassium organotrifluoroborate compound can be produced in a single reaction without recourse to a process of isolating and purifying an intermediate. The novel potassium organotrifluoroborate compound having a hydroxyl group is useful as a reactant which is widely used in the total synthesis of physiologically active natural products and diverse organic synthesis reactions including halogen substitution reactions, 1,2- and 1,4-addition reactions using a rhodium (Rh) catalyst, and Suzuki coupling reactions using a palladium (Pd) catalyst.
专利号:CN-111170926-B 优先权日:2020-01-10 标题:Method for catalyzing asymmetric synthesis of chiral beta-alkynyl-beta-aminoketone derivative
专利号:CN-111170926-A 优先权日:2020-01-10 标题 :A method for catalytic asymmetric synthesis of chiral β-alkynyl-β-amino ketone derivatives
参考标题:α-Phosphonovinyl Arylsulfonates: An Attractive Partner For The Synthesis Of α-Substituted Vinylphosphonates Through Palladium-Catalyzed Suzuki Reactions 作者:Yewen Fang,Li Zhang,Xiaoping Jin,Jinjian Li,Meijuan Yuan,Ruifeng Li,Tong Wang,Tao Wang,Hanjun Hu,Juejun Gu |发布日期:2016.3 摘要:A New And Attractive Coupling Partner For The Synthesis Of α‐substituted Vinylphosphonates Through Suzuki Reactions Has Been Developed. The Developed O‐centered Electrophiles Couple With Various Organoboron Reagents To Give α‐substituted Vinylphosphonates In Moderate To Excellent Yields. This Protocol Features Broad Substrate Scope, Mild Conditions, And High Efficiency.
合成参考文献
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